87967-95-1Relevant academic research and scientific papers
Dimeric isoxazolyl-1,4-dihydropyridines have enhanced binding at the multi-drug resistance transporter
Steiger, Scott A.,Li, Chun,Backos, Donald S.,Reigan, Philip,Natale
supporting information, p. 3223 - 3234 (2017/05/29)
A series of dimeric isoxazolyl-1,4-dihydropyridines (IDHPs) were prepared by click chemistry and examined for their ability to bind the multi-drug resistance transporter (MDR-1), a member of the ATP-binding cassette superfamily (ABC). Eight compounds in t
Chiral Mercaptoacetamides Display Enantioselective Inhibition of Histone Deacetylase6 and Exhibit Neuroprotection in Cortical Neuron Models of Oxidative Stress
Kalin, Jay H.,Zhang, Hankun,Gaudrel-Grosay, Sophie,Vistoli, Giulio,Kozikowski, Alan P.
, p. 425 - 439 (2012/06/04)
Mercaptoacetamide-based ligands have been designed as a new class of histone deacetylase (HDAC) inhibitors for possible use in the treatment of neurodegenerative diseases. The thiol group of these compounds provides a key binding element for interaction with the catalytic zinc ion, and thus differs from the more typically employed hydroxamic acid based zinc binding groups. Herein we disclose the chemistry and biology of some substituted mercaptoacetamides with the intention of increasing HDAC6 isoform selectivity while maintaining potency similar to their hydroxamic acid analogues. The introduction of a stereocenter α to the thiol group was found to have a considerable impact on HDAC inhibitor potency. These new compounds were also profiled for their therapeutic potential in an invitro model of stress-induced neuronal injury and were found to act as nontoxic neuroprotective agents.
ISOXAZOLES / O-PYRIDINES WITH ETHYL AND ETHENYL LINKER
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Page/Page column 11, (2010/09/05)
The present invention is concerned with novel isoxazole-pyridines of formula I wherein R1, R2, R3 and L are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the
ISOXAZOLE-PYRAZOLE DERIVATIVES
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Page/Page column 133; 134, (2010/11/18)
The present invention is concerned with isoxazole-pyrazole derivatives of formula I, having affinity and selectivity for GABA A α5 receptor, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.
Highly substituted isoxazoles: The Baylis-Hillman reaction of substituted 4-isoxazolecarbaldehydes and attempted cyclization to isoxazole-annulated derivatives
Roy, Amrendra K.,Batra, Sanjay
, p. 1347 - 1356 (2007/10/03)
In an attempt to understand the effect of position of the formyl group on the efficiency of Baylis-Hillman reaction within isoxazolecarbaldehydes, the reactions of substituted 4-isoxazolecarbaldehydes to obtain highly substituted isoxazoles are described. Attempts to obtain isoxazole-annulated derivatives from these Baylis-Hillman adducts involving SNR′-SNAr substitution strategy are also described.
Cycloadditions of nitrile oxides to α,β-unsaturated aldehydes. Frontier orbital interactions and secondary orbital interactions at work in determining regiochemistry
Toma, Lucio,Quadrelli, Paolo,Perrini, Giancarlo,Gandolfi, Remo,Di Valentin, Cristiana,Corsaro, Antonino,Caramella, Pierluigi
, p. 4299 - 4309 (2007/10/03)
The regiochemistry of the cycloadditions of nitrile oxides to crotonaldehyde and cinnamaldehyde has been determined and is dictated by frontier orbital interactions and secondary orbital interactions as well. In cycloadditions to α,β-unsaturated compounds the directive effect of the frontier orbital interactions can be diverted by steric drifts and secondary orbital interactions. (C) 2000 Elsevier Science Ltd.
Eine verbesserte Methode zur Synthese substituierter Isoxazol-4-carbaldehyde
Heck, Reinhard,Ofenloch, Roland,Wolf, Roland
, p. 62 - 64 (2007/10/02)
A series of isoxazole-4-carbaldehydes 3 have been readily prepared by simple oxidation of the corresponding isoxazolylalcohols 2 with sodium dichromate in dimethylsulfoxide.
NEUTRAL DICHROMATE OXIDATION. PREPARATION AND UTILITY OF ISOXAZOLE ALDEHYDES
Natale, Nicholas R.,Quincy, David A.
, p. 817 - 822 (2007/10/02)
Isoxazole alcohols 1 can be oxidized by potassium dichromate in neutral organic media to give the corresponding aldehydes, 2 without destruction of the isoxazole ring.Isoxazole aldehydes 2 are of utility as starting materials for 4-(4'-isoxazyl)-1,4-dihydropyridines 3.
